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| 5mg |
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| 10mg |
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| Targets |
gamma-2-MSH (41-58), amide targets melanocortin receptors, which are part of the G protein-coupled receptor (GPCR) family. As a melanocortin endogenous agonist ligand, the peptide contains the conserved His-Phe-Arg-Trp motif that is essential for binding to melanocortin receptors. The melanocortin system includes five receptor subtypes (MC1R through MC5R) that are involved in a variety of physiological functions including pigmentation, energy homeostasis, inflammation, and steroidogenesis. gamma-2-MSH is derived from the N-terminal fragment of proopiomelanocortin (POMC), a precursor protein that also gives rise to other melanocortin peptides such as ACTH, alpha-MSH, and beta-MSH. The specific receptor subtype selectivity of gamma-2-MSH (41-58), amide has not been fully characterized in the available literature.
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| ln Vitro |
In vitro activity data for gamma-2-MSH (41-58), amide are limited. As a melanocortin receptor agonist, the peptide is expected to bind to melanocortin receptors and activate downstream signaling pathways. The conserved His-Phe-Arg-Trp motif is critical for receptor binding and activation. gamma-2-MSH is derived from the N-terminal fragment of POMC and contains this motif common to all melanocortin endogenous agonist ligands. However, specific in vitro activity data such as binding affinities, receptor selectivity, or functional potency (EC₅0 values) have not been extensively reported in the available literature. The compound's activity in cell-based systems would involve activation of melanocortin receptors and downstream signaling via cAMP or other second messengers. Further characterization is needed to establish its pharmacological profile.
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| ln Vivo |
In vivo activity data for gamma-2-MSH (41-58), amide are limited. As a melanocortin receptor agonist derived from POMC, the peptide may exert effects on various physiological processes regulated by the melanocortin system, including energy homeostasis, inflammation, and pigmentation. However, comprehensive in vivo studies evaluating the compound's effects in animal models have not been extensively reported in the available literature. The compound is a 12-amino acid peptide with a molecular weight of 1569.79, which may limit its oral bioavailability and require parenteral administration for in vivo studies. Further research is needed to establish the compound's in vivo efficacy, pharmacokinetics, and safety profile.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for gamma-2-MSH (41-58), amide typically involves measuring its binding affinity to melanocortin receptors using radioligand binding assays. The assay system includes membranes prepared from cells expressing melanocortin receptors (such as MC1R, MC3R, MC4R, or MC5R) and a radiolabeled ligand (such as [¹2⁵I]-NDP-alpha-MSH). gamma-2-MSH (41-58), amide is added at varying concentrations (typically 0.1 nM to 10 uM) and incubated with the receptor membranes in binding buffer (containing Tris-HCl, BSA, and protease inhibitors) at room temperature or 37degC for 1-2 hours. Bound and free radioligand are separated by filtration or centrifugation, and radioactivity is measured using a gamma counter. Binding affinity (IC₅0 or Ki) is calculated from competition binding curves using nonlinear regression analysis.
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| Cell Assay |
The in vitro cell-based assay for gamma-2-MSH (41-58), amide involves culturing cells expressing melanocortin receptors, such as HEK293 or CHO cells stably or transiently transfected with MC1R, MC3R, MC4R, or MC5R. Cells are typically seeded in multi-well plates and treated with varying concentrations of the peptide (0.1 nM to 10 uM) for 30-60 minutes at 37degC. Following treatment, the activation of melanocortin receptors is assessed by measuring cAMP accumulation using ELISA or homogeneous time-resolved fluorescence (HTRF) assays. Alternatively, downstream signaling can be evaluated by measuring CREB phosphorylation or reporter gene assays (such as CRE-luciferase). Cell viability is assessed using standard assays to ensure that observed effects are not due to cytotoxicity. The compound's sequence is YVMGHFRWDRFG-NH2.
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| Animal Protocol |
In vivo animal studies for gamma-2-MSH (41-58), amide have not been extensively documented in the literature. Based on the compound's mechanism as a melanocortin receptor agonist derived from POMC, potential animal studies would typically involve administration of the peptide via intravenous, intraperitoneal, or subcutaneous routes in rodent models to assess its effects on energy homeostasis, inflammation, or other melanocortin-regulated processes. Dosing would be determined based on preliminary pharmacokinetic data and solubility profiles. Common endpoints in such studies would include evaluation of food intake, body weight, metabolic parameters, and inflammatory markers. However, comprehensive in vivo efficacy and toxicity studies have not been widely reported for this compound. The peptide's 12-amino acid sequence (YVMGHFRWDRFG-NH2) may limit oral bioavailability.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of gamma-2-MSH (41-58), amide have not been characterized in the literature. The compound has a molecular weight of 1569.79 g/mol and a molecular formula of C₇4H100N22O1₅S. The peptide sequence is YVMGHFRWDRFG-NH2. As a 12-amino acid peptide, gamma-2-MSH (41-58), amide is likely susceptible to proteolytic degradation in biological systems, which would limit its oral bioavailability and stability in vivo. The compound is a solid and should be stored at -20degC, protected from light, dry, and sealed. For research use, the compound is typically dissolved in DMSO. However, detailed pharmacokinetic parameters such as half-life, clearance, volume of distribution, and bioavailability have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for gamma-2-MSH (41-58), amide are limited, as the compound is a research-use peptide and has not undergone extensive toxicological characterization. Standard safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment such as gloves and lab coats to prevent skin contact and inhalation of dust. The compound should be handled in a well-ventilated area. In case of accidental exposure, rinse affected areas with plenty of water and seek medical attention if irritation persists. Proper waste disposal procedures should be observed in accordance with local regulations. As with all research chemicals, exposure should be minimized and the compound should be stored securely at -20degC, protected from light, dry, and sealed away from incompatible materials.
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| References | |
| Additional Infomation |
gamma-2-MSH (41-58), amide (CAS#: 799841-81-9) is a research-grade peptide with the molecular formula C₇4H100N22O1₅S and a molecular weight of 1569.79. The peptide sequence is YVMGHFRWDRFG-NH2. gamma-2-MSH is a twelve-amino acid peptide derived from the N-terminal fragment of proopiomelanocortin (POMC) and contains the His-Phe-Arg-Trp motif common to all melanocortin endogenous agonist ligands. The compound targets melanocortin receptors and is used in research focused on the melanocortin system and its role in energy homeostasis, inflammation, and other physiological processes. The compound is a solid and should be stored at -20degC, protected from light, dry, and sealed. It is intended for research purposes only. No clinical trials or regulatory approvals have been reported.
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| Molecular Formula |
C74H100N22O15S
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|---|---|
| Molecular Weight |
1569.79
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| Exact Mass |
1570.761
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| CAS # |
799841-81-9
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| PubChem CID |
170907787
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| Appearance |
White to off-white solid powder
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| LogP |
-2.7
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| Hydrogen Bond Donor Count |
24
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| Hydrogen Bond Acceptor Count |
21
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| Rotatable Bond Count |
49
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| Heavy Atom Count |
112
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| Complexity |
3090
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CCSC)C(=O)NCC(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC3=CNC4=CC=CC=C43)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC5=CC=CC=C5)C(=O)NCC(N)O)NC(=O)[C@H](CC6=CC=C(C=C6)O)N
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| InChi Key |
QWPWMCJBQCOTLO-ADJCMCGTSA-N
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| InChi Code |
InChI=1S/C74H102N22O15S/c1-41(2)62(96-63(102)49(75)30-44-22-24-47(97)25-23-44)72(111)91-53(26-29-112-3)64(103)86-39-60(99)88-57(34-46-37-81-40-87-46)70(109)93-55(32-43-16-8-5-9-17-43)68(107)89-52(21-13-28-83-74(79)80)67(106)94-56(33-45-36-84-50-19-11-10-18-48(45)50)69(108)95-58(35-61(100)101)71(110)90-51(20-12-27-82-73(77)78)66(105)92-54(65(104)85-38-59(76)98)31-42-14-6-4-7-15-42/h4-11,14-19,22-25,36-37,40-41,49,51-59,62,84,97-98H,12-13,20-21,26-35,38-39,75-76H2,1-3H3,(H,81,87)(H,85,104)(H,86,103)(H,88,99)(H,89,107)(H,90,110)(H,91,111)(H,92,105)(H,93,109)(H,94,106)(H,95,108)(H,96,102)(H,100,101)(H4,77,78,82)(H4,79,80,83)/t49-,51-,52-,53-,54-,55-,56-,57-,58-,59?,62-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S)-1-[[(2S)-1-[(2-amino-2-hydroxyethyl)amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylbutanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-oxobutanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6370 mL | 3.1851 mL | 6.3703 mL | |
| 5 mM | 0.1274 mL | 0.6370 mL | 1.2741 mL | |
| 10 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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